Name: ShK-235
Brand: Alomone Labs
SKU: STS-380

Overview

Cat #: STS-380

Lyophilized Powder yes

Origin Stichodactyla helianthus (Sun anemone) (Stoichactis helianthus)

Source Synthetic peptide

MW: 4107.9 Da

Purity: >98%

Form Lyophilized Powder

Effective concentration 0.05 – 0.5 nM

Sequence RSCIDTIPKSRCTAFKCKHSIKYRLSFCRKTCGTCA-OH

Modifications Disulfide bonds location- Cys³-Cys³⁵, Cys¹²-Cys²⁸and Cys¹⁷-Cys³²

Structure

Molecular formula C₁₇₄H₂₈₅N₅₅O₄₈S₆

Activity ShK-235 is a potent blocker of K_v1.3 voltage-gated K⁺ channels that exhibits a 2250-fold selectivity for K_v1.3 over K_v1.1 channels¹.

References-Activity

Pennington, M. W. et al. (2015) Mar. Drugs, 13, 529.

Shipping and storage The product is shipped as a lyophilized powder at room temperature. Upon receipt, store the products at -20°C. Protect from moisture.

Solubility Soluble in water. Centrifuge all product preparations before use (10000 x g, 5 min). For long-term storage in solution, we highly recommend preparing a stock solution in pure water (e.g., double-distilled water (ddH2O) at a concentration between 100-1000x of the final working concentration. Divide the solution into small aliquots and store at -20°C. Upon use, thaw the relevant vial and dilute in your working buffer. The preparation of fresh solutions in working buffers before use is recommended. Avoid multiple freeze-thaw cycles to maintain biological activity. Centrifuge all product preparations before use (10000 x g, 5 min).

Storage of solutions The reconstituted solution can be stored at 4°C for up to 1 week. For longer periods (up to 6 months), small aliquots should be stored at -20°C. We do not recommend storing the product in working solutions for longer than a few days. Avoid multiple freeze-thaw cycles.

Our bioassay

Alomone Labs ShK-235 blocks K_V1.3 channels expressed in Xenopus oocytes.
A. Representative time course of ShK-235 (#STS-380) inhibition of normalized K_V1.3 current. Membrane potential was held at -80 mV, current was elicited by a 100 ms voltage ramp to +60 mV every 10 sec, and significantly inhibited by 0.1 nM (green) ShK-235. B. Superimposed traces of K_V1.3 channel currents in the absence (control) and presence of 0.1 nM (green) ShK-235 (taken from the recording in A).

References - Scientific background

Castaneda, O. et al. (1995) Toxicon, 33, 603.
Kalman,K. et al. (1998) J. Biol. Chem., 273, 32697.
Pennington, M. W. et al. (2015) Mar. Drugs, 13, 529.
Chandy, K.G. et al. (2017) Curr. Opin. Chem. Biol., 38, 97.
Pennington, M. W. et al. (2009) Mol. Pharmacol., 75, 762.
Cahalan, M.D. et al. (2009) Immunol. Rev., 231, 59.

Scientific background

ShK-235 is a synthetic analog of ShK (Stichodactyla Toxin) (#STS-400), a native 35 amino acid peptidyl toxin originally isolated from the nematocyst of the sea anemone Stichodactyla helianthus¹. Native ShK blocks the voltage-gated potassium (K_V)1.3, K_V1.1, K_V1.4, and K_V1.6 at subnanomolar concentrations². Its synthetic analog, ShK-235, is a highly specific K_V1.3 blocker with picomolar affinity and exhibited greater than 2250-fold selectivity for K_V1.3 over K_V1.1 and with very little block of other important K_V subtypes (K_V1.4 and K_V1.6)³.

K_v channels play key roles in human physiology and pathology. The K_v1.3 channel in T lymphocytes is a validated therapeutic target for diverse autoimmune diseases⁴. This channel maintains the membrane potential of a sub-set of T lymphocytes known as effector memory (T_EM) T cells, that mediate and play a major role in the pathogenesis of autoimmune diseases such as multiple sclerosis (MS), type 1 diabetes mellitus, rheumatoid arthritis (RA), and psoriasis^5,6.

Target K_v1.3

Lyophilized Powder

ShK-235 (#STS-380) is a highly pure, synthetic, and biologically active peptide toxin.

Certificate of Analysis SDS

For research purposes only, not for human use

Last Update: 04/11/2024

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ShK-235

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Scientific Background

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